印度恩替卡韦

【印度恩替卡韦说明书，怎么吃？】

恩替卡韦（印度）又名恩替卡韦 Entecavir，恩替卡韦适用于恩替卡韦适用于病毒复制活跃、血清转氨酶ALT持续升高或肝脏组织学显示有活动性病变的慢性成年人乙型肝炎的治疗。的治疗，恩替卡韦用法及注意事项,:【用法用量】 1）成年人和16岁以上青少年口服恩替卡韦，每天一次恩替卡韦，每次恩替卡韦0.5mg。 2）拉米夫定治疗时发生病毒血症或出现拉米夫定耐药突变的患者为每天一次恩替卡韦，恩替卡韦每...

【用法用量】
 
1）成年人和16岁以上青少年口服恩替卡韦，每天一次恩替卡韦，每次恩替卡韦0.5mg。
 
2）拉米夫定治疗时发生病毒血症或出现拉米夫定耐药突变的患者为每天一次恩替卡韦，恩替卡韦每次恩替卡韦1.0mg(恩替卡韦0.5mg 两片)。
 
 
 
【不良反应】
 
ALT升高、疲劳、眩晕、恶心、腹痛、腹部不适、上腹痛、肝区不适、肌痛、失眠和风疹。
   
【注意事项】
 
1）患者应在医生的指导下服用恩替卡韦，并告知医生任何新出现的症状及合并恩替卡韦用药情况。医生应告知患者恩替卡韦停药有时会出现肝脏病情加重，所以应在医生的指导下改变治疗方法。
 
2）使用恩替卡韦治疗并不能降低经性接触或污染血源传播HBV的危险性，因此，需要采取适当的防护措施。
 
3）核苷类药物在单独或与其他抗逆转录病毒药物联合使用时，已经有乳酸性酸中毒和重度的脂肪性肝肿大，包括死亡病例的报道。
 
4）当慢性乙肝病人停止抗乙肝治疗后，包括恩替卡韦在内，已经发现有重度急性肝炎发作的报道。对那些停止抗乙肝治疗的病人的肝功能情况应从临床和实验室检查等方面严密监察，并且至少随访数月。如必要，可重新恢复抗乙肝病毒的治疗。
 
 
【特殊人群用药】
 
1）孕妇及哺乳期妇女用药
 
恩替卡韦对妊娠妇女影响的研究尚不充分。只有当对胎儿潜在的风险利益作出充分的权衡后，方可使用恩替卡韦。
 
目前尚无资料提示恩替卡韦能影响HBV的母婴传播，因此，应采取适当的干预措施以防止新生儿感染HBV。
 
恩替卡韦可从大鼠乳汁分泌。但恩替卡韦人乳中是否有分泌仍不清楚，所以不推荐服用恩替卡韦的母亲哺乳。
 
2）儿童用药
 
16岁以下儿童患者使用恩替卡韦的安全性和恩替卡韦有效性数据尚未建立。
 
3）老年用药
 
恩替卡韦由于没有足够的65岁及以上的老年患者参加恩替卡韦的临床研究，尚不清楚老年患者与年轻患者对恩替卡韦的反应有何不同。恩替卡韦其他的临床试验报告也未发现老年患者与年轻患者之间的不同。恩替卡韦主要由肾脏排泄，恩替卡韦在肾功能损伤的患者中，可能发生毒性反应的危险性更高。因为老年患者多数肾功能有所下降，因此应注意恩替卡韦药物剂量的选择，并且监测肾功能。


USES OF ENTAVIR TABLET
Chronic hepatitis B virus (HBV) infection

ENTAVIR TABLET SIDE EFFECTS
Common
Headache
Dizziness
Tiredness
Nausea

HOW TO USE ENTAVIR TABLET
Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Entavir 0.5 mg Tablet is to be taken empty stomach.

HOW ENTAVIR TABLET WORKS
Entavir 0.5 mg Tablet is an antiviral medication. It prevents the multiplication of virus in human cells. This stops the virus from producing new viruses and clears up your infection.

ENTAVIR TABLET RELATED WARNINGS
warnings
Alcohol
Interaction with alcohol is unknown. Please consult your doctor.

warnings
Pregnancy
WEIGH RISKS VS BENEFITS
Entavir 0.5 mg Tablet may be unsafe to use during pregnancy.
Animal studies have shown adverse effects on the fetus, however, there are limited human studies. The benefits from use in pregnant women may be acceptable despite the risk. Please consult your doctor.

warnings
Lactation
CAUTION
Entavir 0.5 mg Tablet is probably unsafe to use during lactation. Limited human data suggest that the drug could represent a significant risk to the baby.

warnings
Driving
Entavir 0.5 mg Tablet may make you feel dizzy, sleepy, tired, or decrease alertness. If this happens, do not drive.

warnings
Kidney
CAUTION
Entavir 0.5 mg Tablet should be used with caution in patients with kidney disease. Dose adjustment of Entavir 0.5 mg Tablet may be needed. Please consult your doctor.

warnings
Liver
SAFE
Entavir 0.5 mg Tablet is safe to use in patients with liver disease. No dose adjustment of Entavir 0.5 mg Tablet is recommended.
WHAT IF YOU MISS A DOSE OF ENTAVIR TABLET?
If you miss a dose of Entavir 0.5 mg Tablet, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.

Entecavir

生物活性

产品描述	Entecavir is a guanosine nucleoside analogue used in the treatment of chronic hepatitis B virus (HBV) infection. Entecavir therapy can be associated with flares of the underlying hepatitis B during or after therapy, but has not been linked to cases of clinically apparent liver injury.
靶点活性	HBV( HepG2 cell),EC50:3.75nM
体外活性	BMS-200475 has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1]. Entecavir is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2].
体内活性	Daily oral treatment with BMS-200475 at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks[3].
细胞实验	BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1].

化学信息

分子量	277.28
分子式	C12H15N5O3
CAS	142217-69-4
溶解度	DMSO: ≥44 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )
储存条件	store at -80°C
备注	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

	1 mg	5 mg	10 mg
1 mM	3.606 ml	18.032 ml	36.065 ml
5 mM	0.721 ml	3.606 ml	7.213 ml
10 mM	0.361 ml	1.803 ml	3.606 ml
50 mM	0.072 ml	0.361 ml	0.721 ml

参考文献
 
1. Sham, H., Kempf, D., Molla, A., Marsh, K., Kumar, G., & Chen, C. et al. (1998). ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease.?Antimicrobial Agents And Chemotherapy,?42(12), 3218-3224. doi: 10.1128/aac.42.12.3218